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Research ArticleArticle

In Vitro Pharmacologic Profile of YM158, a New Dual Antagonist for LTD4 and TXA2 receptors

Yasuhito Arakida, Kiyomi Suwa, Keiko Ohga, Masaki Yokota, Keiji Miyata, Toshimitsu Yamada and Kazuo Honda
Journal of Pharmacology and Experimental Therapeutics November 1998, 287 (2) 633-639;
Yasuhito Arakida
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Kiyomi Suwa
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Keiko Ohga
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Masaki Yokota
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Keiji Miyata
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Toshimitsu Yamada
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Kazuo Honda
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Abstract

YM158 (3-[(4-tert-butylthiazol-2-yl)methoxy]-5′-[3-(4-chlorobenzenesulfonyl) propyl]-2′-(1H-tetrazol-5-ylmethoxy)benzanilide monosodium salt monohydrate) antagonizes leukotriene (LT) D4 and thromboxane (TX) A2 receptors. Functional assays in vitro showed that YM158 exhibits competitive dual antagonism of LTD4 and TXA2 receptor-mediated contraction of isolated guinea pig tracheae, with pA2 values of about 8.87 and 8.81, respectively. Its antagonistic activity for the LTD4 receptor was approximately 6.5 times less potent than that of montelukast, and that for the TXA2 receptor was 2.5 times more potent than that of seratrodast. YM158 also inhibited PGD2- and PGF2α-induced tracheal contractions. YM158 showed no antagonism against LTC4-, histamine- or carbachol-induced contractions of guinea pig tracheae. Furthermore, YM158 antagonized the stable TXA2 analog U46619-induced aggregation of both guinea pig and human platelets and inhibited the LTD4-induced contraction of guinea pig ileum. From these results, YM158 appears to be a novel, selective dual antagonist for both LTD4 and TXA2 receptors.

Footnotes

  • Send reprint requests to: Yasuhito Arakida, Inflammation Research Pharmacology Laboratories, Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd. 21, Miyukigaoka, Tsukuba-shi, Ibaraki 305-8585, Japan.

  • Abbreviations:
    LT
    leukotriene
    Cys-LTs
    cysteinyl-leukotrienes (LTC4, LTD4 and LTE4)
    TX
    thromboxane
    PG
    prostaglandin
    PRP
    platelet-rich plasma
    PPP
    platelet-poor plasma
    IC50
    concentration causing 50% inhibition
    EC50
    concentration causing 50% effect
    YM158
    (3-[(4-tert-butylthiazol-2-yl)methoxy]-5′-[3-(4-chlorobenzenesulfonyl)propyl-2′-(1H-tetrazol-5-ylmethoxy)benzanilide monosodium salt monohydrate)
    • Received January 7, 1998.
    • Accepted June 17, 1998.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics
Vol. 287, Issue 2
1 Nov 1998
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Research ArticleArticle

In Vitro Pharmacologic Profile of YM158, a New Dual Antagonist for LTD4 and TXA2 receptors

Yasuhito Arakida, Kiyomi Suwa, Keiko Ohga, Masaki Yokota, Keiji Miyata, Toshimitsu Yamada and Kazuo Honda
Journal of Pharmacology and Experimental Therapeutics November 1, 1998, 287 (2) 633-639;

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Research ArticleArticle

In Vitro Pharmacologic Profile of YM158, a New Dual Antagonist for LTD4 and TXA2 receptors

Yasuhito Arakida, Kiyomi Suwa, Keiko Ohga, Masaki Yokota, Keiji Miyata, Toshimitsu Yamada and Kazuo Honda
Journal of Pharmacology and Experimental Therapeutics November 1, 1998, 287 (2) 633-639;
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